Rebastinib

Rebastinib is a potent ABL1 kinase inhibitor that binds to amino acid residues that are used to switch between active and inactive conformations. It inhibits both phosphorylated and unphosphorylated ABL1 as well as gatekeeper mutant T315I. Rebastinib was active against chronic myeloid leukemia Ba/F3 cells expressing BCR-ABL and BCR-ABLT315I and most kinase mutants. Rebastinib has been reported to inhibit the growth and metastasis of xenografted MDA-MB-231 triple-negative breast cancer cells by targeting AXL/MET. It has also been shown to be a potent inhibitor of Tie2 kinase. Rebastinib blocked necroptosis via inhibition of RIPK1 and RIPK3.